Thalitero 100 mg | Thalidomide | Blueberry pharmacaeuticals
THALITERO 100MG
Thalitero 100mg is a piperidinyl isoindole basically introduced as a non-barbiturate hypnotic but detached from the market due to teratogenic effects. It has been renewing and indicated for several immunological and inflammatory disorders. Thalitero 100mg displays immunosuppressive and anti-angiogenic activity. It prevents release of tumor necrosis factor-alpha from monocytes and modulates another cytokine action.
Indication :
Thalitero 100mg is used for the acute treatment of the cutaneousmanifestations of moderate to severe erythema nodosum leprosum (ENL).
Thalitero 100mg is not used as monotherapy for such ENL treatment in the presence of moderate to severe neuritis. Thalitero 100mg in combination with dexamethasone is indicated for the treatment of patients with newly diagnosed multiple myeloma.
Thalitero 100mg is also used as maintenance therapy for prohibition and suppression of the cutaneous manifestations of ENL relapsed.
Mechanism of Action :
The immunologic effects of thalidomide vary considerably under different conditions but may be related to overthrow of exaggerated tumor necrosis factor-alpha (TNF-a) production and down-modulation of selected cell surface adhesion molecules involved in leukocyte migration.
For example, patients getting of thalidomide has been resulted to reduce circulating levels of TNF-a in patients with ENL, however, it has also been shown to increase plasma TNF-a levels in HIV-sero positive patients. Since cancer therapy, the medication may work as a VEGF inhibitor.
Pharmacokinetic :
Absorption :
Time to peak plasma concentration is 2.9 to 5.7 hours
Distribution :
plasma protein binding is 55% and 66% for the (+) R and (-) S enantiomers, respectively
Metabolism :
Metabolized hepatically by enzymes of the cytochrome P450 enzyme system.
Elimination :
Excreted in the urine as unchanged drug is less than 0.7% of the dose. Half-life of thalidomide is 5 to 7 hours.
Dosage And Administration :
The dosage recommendation of following condition as follows :
Multiple Myeloma :
The recommended dose is 200mg PO qHS in 28-day cycles
Administer 40 mg of dexamethasone on days 1-4,9-12,17-20 of 28 days.
Erythema Nodosum leprosum :
The initial recommended dose is 100-300 mg PO qHS.
In case of more severe reaction then may initiate at 400mg. continue until active symptoms subsided, at least 2 weeks then titrate down by 50 mg increment q 2-4 weeks.
DRUG INTERACTION :
Interaction of Thalitero 100mg with cardiovascular medication will cause an additive bradycardic effect and should be used with caution.
Combination with bortezomib, amiodarone, cisplatin, docetaxel, paclitaxel, vincristine etc will cause peripheral neuropathy and should be used with caution.
Unknown condition when concomitant use of hormonal contraceptives further increases the risk of thromboembolism with Thalitero 100mg.
Contraindication:
Hypersentivity
Pregnancy - the drug cause risk to fetal..
Pregnancy :
If a woman becomes pregnant during Thalitero therapy, the drug must be discontinued immediately, and the woman given correct counselling.
Pregnancy category X: Thalitero 100mg may cause risk to fetal when administer to a pregnant woman. This drug should not administer to a pregnant woman or a woman who aims to become pregnant.
Lactation :
If a woman becomes pregnant during Thaliterotherapy, the drug must be discontinued immediately, and the woman given correct counselling.
Pregnancy category X: Thalitero 100mg may cause risk to fetal when administer to a pregnant woman. This drug should not administer to a pregnant woman or a woman who aims to become pregnant.
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